Article
Design, synthesis and biological evaluation of imine-containing inhibitors against the triple-mutant EGFR kinases based on the scaffold of osimertinib.
Bioorganic chemistry - 15 Jun 2025
Ding Shi, Wu Yuanyu, Li Bin, Wang Xin, Ding Haotian, Zhan Zhenzhen, Shen Jiwei, Qi Rui, Gao Ziye, Yao Kai, Su Riya, Zheng Hanxue, Tang Zhongyu, Liu Ju, Chen Ye
Abstract excerpt
A series of EGFR inhibitors were designed and synthesized based on the scaffold of osimertinib, the inhibitory activities against the L858R/T790M/C797S mutant EGFR kinase of which were subsequently evaluated. Compounds with the imine fragments showed the highest kinase inhibitory activity and were proved to be reversible inhibitors, which were represented by the compound DD-8 (IC50 = 0.87 nM). Kinase selectivity...
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